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Compound Detail

CHEMBL131777

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C=CCn1ncc(C2CCCNC2)n1

Basic Information

ChEMBL ID CHEMBL131777
Phase Preclinical
Structure Type MOL
InChI Key WUDWCZHMLGCBCZ-UHFFFAOYSA-N
5
Targets
17
Activities
2
Assay Types
0
PK Parameters
6
Publications
0
Known Names

Molecular Properties

192.3
MW (Da)
0.93
ALogP
4
HBA
1
HBD
42.7
PSA (Ų)
0.72
QED
0
Ro5 Violations
3
Rot. Bonds

Drug Information

Molecule Type Small molecule
Availability Unknown
Chirality Unknown

Flags

First in Class Prodrug

Extended Properties

Molecular Formula C10H16N4
MW 192.27
Aromatic Rings 1
Heavy Atoms 14
NP-Likeness -0.83

Activity Summary

Ki 12 meas. best 7.6
EC50 5 meas. best 6.17

Target Activity Profile

Target Type Best pChEMBL Mean pChEMBL Best (nM) # Data
Muscarinic acetylcholine receptor
CHEMBL1907609
Ki 7.6 6.77 25.0 9
Muscarinic acetylcholine receptor M1
CHEMBL276
Ki 7.0 6.8167 100.0 3
Muscarinic acetylcholine receptor M2
CHEMBL211
EC50 6.17 6.07 680.0 3
Muscarinic acetylcholine receptors; M2 & M3
CHEMBL2095187
EC50 5.37 5.37 4300.0 1
Muscarinic acetylcholine receptor M3
CHEMBL5498
EC50 5.36 5.36 4400.0 1

Activity Data Samples

Top measurements by pChEMBL value

Target Type Rel. Value Units pChEMBL Assay PubMed
Muscarinic acetylcholine receptor Ki = 25.0 nM 7.6 In vitro binding affinity for muscarinic receptor by displacing [3H]oxotremorine... 7990109
Muscarinic acetylcholine receptor Ki = 37.0 nM 7.43 In vitro binding affinity for muscarinic receptor by displacing [3H]oxotremorine... 7990109
Muscarinic acetylcholine receptor Ki = 45.0 nM 7.35 In vitro binding affinity for muscarinic receptor by displacing [3H]oxotremorine... 7990109
Muscarinic acetylcholine receptor M1 Ki = 100.0 nM 7.0 In vitro binding affinity for muscarinic M1 receptor by displacing [3H]pirenzepi... 7990109
Muscarinic acetylcholine receptor M1 Ki = 170.0 nM 6.77 In vitro binding affinity for muscarinic M1 receptor by displacing [3H]pirenzepi... 7990109
Muscarinic acetylcholine receptor Ki = 190.0 nM 6.72 In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidiny... 7990109
Muscarinic acetylcholine receptor M1 Ki = 210.0 nM 6.68 In vitro binding affinity for muscarinic M1 receptor by displacing [3H]pirenzepi... 7990109
Muscarinic acetylcholine receptor Ki = 300.0 nM 6.52 In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidiny... 7990109
Muscarinic acetylcholine receptor Ki = 310.0 nM 6.51 In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidiny... 7990109
Muscarinic acetylcholine receptor Ki = 330.0 nM 6.48 In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidiny... 7990109
Muscarinic acetylcholine receptor Ki = 530.0 nM 6.28 In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidiny... 7990109
Muscarinic acetylcholine receptor M2 EC50 = 680.0 nM 6.17 M2 agonist activity estimated by depression of isolated guinea pig left atrium 7990109
Muscarinic acetylcholine receptor M2 EC50 = 840.0 nM 6.08 M2 agonist activity estimated by depression of isolated guinea pig left atrium 7990109
Muscarinic acetylcholine receptor Ki = 910.0 nM 6.04 In vitro binding affinity for muscarinic receptor by displacing [3H]quinuclidiny... 7990109
Muscarinic acetylcholine receptor M2 EC50 = 1100.0 nM 5.96 M2 agonist activity estimated by depression of isolated guinea pig left atrium 7990109
Muscarinic acetylcholine receptors; M2 & M3 EC50 = 4300.0 nM 5.37 M2/M3 agonist activity estimated by contraction of isolated guinea pig ileum 7990109
Muscarinic acetylcholine receptor M3 EC50 = 4400.0 nM 5.36 In vitro ability to contract isolated guinea pig ileum was used to estimate M2/M... 7990109

Literature References

PubMed DOI Target Context # Activities
7990109 10.1021/jm00050a006 Muscarinic acetylcholine receptor M2 12
7990109 10.1021/jm00050a006 Muscarinic acetylcholine receptor 9
7990109 10.1021/jm00050a006 Muscarinic acetylcholine receptor M1 6
7990109 10.1021/jm00050a006 Rattus norvegicus 6
7990109 10.1021/jm00050a006 Muscarinic acetylcholine receptor M3 2
7990109 10.1021/jm00050a006 Muscarinic acetylcholine receptors; M2 & M3 1

Data from ChEMBL 36 via Core Engine